SYNTHESIS OF 4-(PHENYLAMINO)QUINOLINE-3-CARBOXAMIDES AS A NOVEL CLASS OF GASTRIC H+/K+-ATPASE INHIBITORS

被引：0
|
作者：
UCHIDA, M
OTSUBO, K
MATSUBARA, J
OHTANI, T
MORITA, S
YAMASAKI, K
机构：
来源：
CHEMICAL & PHARMACEUTICAL BULLETIN | 1995年 / 43卷 / 04期
关键词：
4-(PHENYLAMINO)QUINOLINE-3-CARBOXAMIDE; ANTISECRETORY ACTIVITY; H+ K+-ATPASE INHIBITOR; ANTIULCER ACTIVITY; CYTOPROTECTIVE ACTIVITY; REVERSIBLE INHIBITOR;
D O I：
暂无
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
In a search for inhibitors of gastric H+/K+-ATPase, 4-(phenylamino)quinoline-3-carboxamides were synthesized and evaluated for antisecretory activity against histamine-induced gastric acid secretion in rats. These compounds were synthesized by condensation of aniline derivatives with N-substituted 4-chloroquinoline-3-carboxamides, which were obtained from treatment of 4(1H)-quinolinone-3-carboxylic acid with thionyl chloride. Most of the compounds inhibited histamine-induced gastric acid secretion in rats. Among them, N-allyl-4-(2-ethylphenylamino)quinoline-3-carboxamide (4h) was the most potent inhibitor and had the best profile as a candidate antiulcer agent. This compound showed reversible, K+-competitive gastric H+/K+-ATPase inhibitory activity.
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页码：693 / 698
页数：6
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